期刊
JOURNAL OF NEUROCHEMISTRY
卷 85, 期 3, 页码 779-790出版社
WILEY
DOI: 10.1046/j.1471-4159.2003.01716.x
关键词
ethanol; HEK293 cells; P2X(3) receptor; P2Y(1) receptor; trichloroethanol
Membrane currents and changes in the intracellular Ca2+ concentration ([Ca2+](i)) were measured in HEK293 cells transfected with the human P2X(3) receptor (HEK293-hP2X(3)). RT-PCR and immunocytochemistry indicated the additional presence of endogenous P2Y(1) and to some extent P2Y(4) receptors. P2 receptor agonists induced inward currents in HEK293-hP2X(3) cells with the rank order of potency alpha,beta-meATP approximate to ATP > ADP-beta-S > UTP. A comparable rise in [Ca2+](i) was observed after the slow superfusion of ATP, ADP-beta-S and UTP; alpha,beta-meATP was ineffective. These data, in conjunction with results obtained by using the P2 receptor antagonists TNP-ATP, PPADS and MRS2179 indicate that the current response to alpha,beta-meATP is due to P2X(3) receptor activation, while the ATP-induced rise in [Ca2+](i) is evoked by P2Y(1) and P2Y(4) receptor activation. TCE depressed the alpha,beta-meATP current in a manner compatible with a non-competitive antagonism. The ATP-induced increase of [Ca2+](i) was much less sensitive to the inhibitory effect of TCE than the current response to alpha,beta-meATP. The present study indicates that in HEK293-hP2X(3) cells, TCE, but not ethanol, potently inhibits ligand-gated P2X(3) receptors and, in addition, moderately interferes with G protein-coupled P2Y(1) and P2Y(4) receptors. Such an effect may be relevant for the interruption of pain transmission in dorsal root ganglion neurons following ingestion of chloral hydrate or trichloroethylene.
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